GSK-2816126

Investigational

Details

Stereochemistry	ABSOLUTE
Molecular Formula	C31H38N6O2
Molecular Weight	526.6724
Optical Activity	UNSPECIFIED
Defined Stereocenters	1 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CC[C@H](C)N1C=C(C)C2=C1C=C(C=C2C(=O)NCC3=C(C)C=C(C)NC3=O)C4=CC=C(N=C4)N5CCNCC5

InChI

InChIKey=FKSFKBQGSFSOSM-QFIPXVFZSA-N

InChI=1S/C31H38N6O2/c1-6-22(5)37-18-20(3)29-25(30(38)34-17-26-19(2)13-21(4)35-31(26)39)14-24(15-27(29)37)23-7-8-28(33-16-23)36-11-9-32-10-12-36/h7-8,13-16,18,22,32H,6,9-12,17H2,1-5H3,(H,34,38)(H,35,39)/t22-/m0/s1

HIDE SMILES / InChI

Molecular Formula	C31H38N6O2
Molecular Weight	526.6724
Charge	0
Count

Stereochemistry	ABSOLUTE
Additional Stereochemistry	No
Defined Stereocenters	1 / 1
E/Z Centers	0
Optical Activity	UNSPECIFIED

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/23051747 | https://www.ncbi.nlm.nih.gov/pubmed/26898301
Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/27926488 | https://newdrugapprovals.org/tag/gsk-126/

GSK126, a potent, highly selective, S-adenosyl-methionine-competitive, small-molecule inhibitor of EZH2 methyltransferase activity, decreases global H3K27me3 levels and reactivates silenced PRC2 target genes. GSK126 effectively inhibits the proliferation of EZH2 mutant DLBCL cell lines and markedly inhibits the growth of EZH2 mutant DLBCL xenografts in mice. Pharmacological inhibition of EZH2 activity may provide a promising treatment for EZH2 mutant lymphoma. EZH2 inactivation by GSK126 is also effective in killing MM cells and CSCs as a single agent or in combination with bortezomib. Clinical trial of GSK126 in patients with MM may be warranted. GSK126 is undergoing phase I trials for hypermethylation-related cancers. GSK126 is in phase I diffuse large B cell lymphoma and follicular lymphoma. GSK126 inhibits cell migration and angiogenesis in solid tumor cell lines through down-regulation of VEGF-A expression. Thus, it may be considered as a novel anticancer drug candidate for solid tumor.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Histone-lysine N-methyltransferase EZH2 10 Target ID: CHEMBL2189110 Sources: https://www.ncbi.nlm.nih.gov/pubmed/23051747 \| https://www.ncbi.nlm.nih.gov/pubmed/26189078	Inhibitor 8504		9.9 nM [IC50]
Vascular endothelial growth factor A 3 Target ID: CHEMBL1783 Sources: https://www.ncbi.nlm.nih.gov/pubmed/26898301	Inhibitor 8504

Conditions

Condition	Modality	Highest Phase	Product
Diffuse large B-cell lymphoma 22 Sources: http://adisinsight.springer.com/drugs/800040201 https://clinicaltrials.gov/ct2/show/NCT02082977	Primary	Phase I 438	Unknown Approved Use Unknown
Follicular lymphoma 4 Sources: http://adisinsight.springer.com/drugs/800040201 https://clinicaltrials.gov/ct2/show/NCT02082977	Primary	Phase I 438	Unknown Approved Use Unknown
Multiple myeloma 159 Sources: https://clinicaltrials.gov/ct2/show/NCT02082977	Primary	Phase I 438	Unknown Approved Use Unknown
Solid tumors 147 Sources: https://clinicaltrials.gov/ct2/show/NCT02082977	Primary	Phase I 438	Unknown Approved Use Unknown

C_max

Value	Dose	Analyte	Population
0.42 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31471312/	50 mg 2 times / week multiple, intravenous dose: 50 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	GSK-2816126 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
0.5 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31471312/	50 mg 2 times / week multiple, intravenous dose: 50 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	GSK-2816126 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
1.1 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31471312/	100 mg 2 times / week multiple, intravenous dose: 100 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	GSK-2816126 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
1 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31471312/	100 mg 2 times / week multiple, intravenous dose: 100 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	GSK-2816126 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
1.4 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31471312/	200 mg 2 times / week multiple, intravenous dose: 200 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	GSK-2816126 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
1.5 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31471312/	200 mg 2 times / week multiple, intravenous dose: 200 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	GSK-2816126 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
4 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31471312/	400 mg 2 times / week multiple, intravenous dose: 400 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	GSK-2816126 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
3.5 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31471312/	400 mg 2 times / week multiple, intravenous dose: 400 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	GSK-2816126 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
7.31 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31471312/	800 mg 2 times / week multiple, intravenous dose: 800 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	GSK-2816126 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
7.46 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31471312/	800 mg 2 times / week multiple, intravenous dose: 800 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	GSK-2816126 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
10.9 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31471312/	1200 mg 2 times / week multiple, intravenous dose: 1200 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	GSK-2816126 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
11.6 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31471312/	1200 mg 2 times / week multiple, intravenous dose: 1200 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	GSK-2816126 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
13 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31471312/	1800 mg 2 times / week multiple, intravenous dose: 1800 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	GSK-2816126 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
14.2 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31471312/	1800 mg 2 times / week multiple, intravenous dose: 1800 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	GSK-2816126 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
22.3 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31471312/	2400 mg 2 times / week multiple, intravenous dose: 2400 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	GSK-2816126 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
21.6 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31471312/	2400 mg 2 times / week multiple, intravenous dose: 2400 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	GSK-2816126 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
23.8 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31471312/	3000 mg 2 times / week multiple, intravenous dose: 3000 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	GSK-2816126 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
30.5 μg/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31471312/	3000 mg 2 times / week multiple, intravenous dose: 3000 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	GSK-2816126 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

AUC

Value	Dose	Analyte	Population
1.33 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31471312/	50 mg 2 times / week multiple, intravenous dose: 50 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	GSK-2816126 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
3.9 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31471312/	50 mg 2 times / week multiple, intravenous dose: 50 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	GSK-2816126 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
7 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31471312/	100 mg 2 times / week multiple, intravenous dose: 100 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	GSK-2816126 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
13.2 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31471312/	400 mg 2 times / week multiple, intravenous dose: 400 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	GSK-2816126 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
14.8 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31471312/	400 mg 2 times / week multiple, intravenous dose: 400 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	GSK-2816126 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
26.4 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31471312/	800 mg 2 times / week multiple, intravenous dose: 800 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	GSK-2816126 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
33.3 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31471312/	800 mg 2 times / week multiple, intravenous dose: 800 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	GSK-2816126 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
60.9 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31471312/	1200 mg 2 times / week multiple, intravenous dose: 1200 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	GSK-2816126 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
60.2 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31471312/	1200 mg 2 times / week multiple, intravenous dose: 1200 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	GSK-2816126 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
51.2 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31471312/	1800 mg 2 times / week multiple, intravenous dose: 1800 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	GSK-2816126 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
81.7 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31471312/	1800 mg 2 times / week multiple, intravenous dose: 1800 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	GSK-2816126 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
102 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31471312/	2400 mg 2 times / week multiple, intravenous dose: 2400 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	GSK-2816126 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
123 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31471312/	2400 mg 2 times / week multiple, intravenous dose: 2400 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	GSK-2816126 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
103 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31471312/	3000 mg 2 times / week multiple, intravenous dose: 3000 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	GSK-2816126 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
183 μg × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31471312/	3000 mg 2 times / week multiple, intravenous dose: 3000 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	GSK-2816126 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

T_1/2

Value	Dose	Analyte	Population
7.62 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31471312/	50 mg 2 times / week multiple, intravenous dose: 50 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	GSK-2816126 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
46.5 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31471312/	50 mg 2 times / week multiple, intravenous dose: 50 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	GSK-2816126 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
36.8 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31471312/	100 mg 2 times / week multiple, intravenous dose: 100 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	GSK-2816126 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
49.1 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31471312/	400 mg 2 times / week multiple, intravenous dose: 400 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	GSK-2816126 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
39.7 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31471312/	400 mg 2 times / week multiple, intravenous dose: 400 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	GSK-2816126 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
26.5 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31471312/	800 mg 2 times / week multiple, intravenous dose: 800 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	GSK-2816126 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
27.35 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31471312/	800 mg 2 times / week multiple, intravenous dose: 800 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	GSK-2816126 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
14.1 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31471312/	1200 mg 2 times / week multiple, intravenous dose: 1200 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	GSK-2816126 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
27.3 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31471312/	1200 mg 2 times / week multiple, intravenous dose: 1200 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	GSK-2816126 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
31.8 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31471312/	1800 mg 2 times / week multiple, intravenous dose: 1800 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	GSK-2816126 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
29.88 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31471312/	1800 mg 2 times / week multiple, intravenous dose: 1800 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	GSK-2816126 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
33.7 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31471312/	2400 mg 2 times / week multiple, intravenous dose: 2400 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	GSK-2816126 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
22.75 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31471312/	2400 mg 2 times / week multiple, intravenous dose: 2400 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	GSK-2816126 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
22.5 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31471312/	3000 mg 2 times / week multiple, intravenous dose: 3000 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	GSK-2816126 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN
27.25 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/31471312/	3000 mg 2 times / week multiple, intravenous dose: 3000 mg route of administration: Intravenous experiment type: MULTIPLE co-administered:	GSK-2816126 plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

Doses

Dose	Population	Adverse events
3000 mg 2 times / week multiple, intravenous Highest studied dose Dose: 3000 mg, 2 times / week Route: intravenous Route: multiple Dose: 3000 mg, 2 times / week Sources: https://pubmed.ncbi.nlm.nih.gov/31471312/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/31471312/	DLT: Aspartate aminotransferase increase, ALT increased... Dose limiting toxicities: Aspartate aminotransferase increase (grade 4, 14.3%) ALT increased (grade 2-3, 28.6%) Sources: https://pubmed.ncbi.nlm.nih.gov/31471312/
2400 mg 2 times / week multiple, intravenous MTD Dose: 2400 mg, 2 times / week Route: intravenous Route: multiple Dose: 2400 mg, 2 times / week Sources: https://pubmed.ncbi.nlm.nih.gov/31471312/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/31471312/	Sources: https://pubmed.ncbi.nlm.nih.gov/31471312/

AEs

AE	Significance	Dose	Population
ALT increased	grade 2-3, 28.6% DLT	3000 mg 2 times / week multiple, intravenous Highest studied dose Dose: 3000 mg, 2 times / week Route: intravenous Route: multiple Dose: 3000 mg, 2 times / week Sources: https://pubmed.ncbi.nlm.nih.gov/31471312/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/31471312/
Aspartate aminotransferase increase	grade 4, 14.3% DLT	3000 mg 2 times / week multiple, intravenous Highest studied dose Dose: 3000 mg, 2 times / week Route: intravenous Route: multiple Dose: 3000 mg, 2 times / week Sources: https://pubmed.ncbi.nlm.nih.gov/31471312/	unhealthy, ADULT Health Status: unhealthy Age Group: ADULT Sex: M+F Food Status: UNKNOWN Sources: https://pubmed.ncbi.nlm.nih.gov/31471312/

PubMed

Title	Date	PubMed
Blocking EZH2 methylation transferase activity by GSK126 decreases stem cell-like myeloma cells.	2017-01-10	27926488
The novel EZH2 inhibitor, GSK126, suppresses cell migration and angiogenesis via down-regulating VEGF-A.	2016-04	26898301
EZH2 inhibition as a therapeutic strategy for lymphoma with EZH2-activating mutations.	2012-12-06	23051747

Patents

Sample Use Guides

In Vivo Use Guide

Subject will be administered with a 50 milligram (mg) starting dose of GSK126 intravenous infusion over 2 - 4 hours, initially twice-weekly 3 weeks on / 1 week off in each 28-day cycle. Dose escalation will continue until an RP2D is determined or until an maximum tolerated dose (MTD) or a dose of 3000 mg twice-weekly is reached.

Route of Administration: Intravenous

In Vitro Use Guide

GSK126 showed significant effect on prostate cancer PC-3 and DU145 cell growth and apoptosis when the dose was higher than 50 umol/L.

Substance Class	Chemical Created by `admin` on `Tue Apr 01 16:26:52 GMT 2025` Edited by `admin` on `Tue Apr 01 16:26:52 GMT 2025`
Record UNII	W4OGW9QZ97
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

GSK-126

Preferred Name

English

GSK-2816126

Common Name

English

GSK-2816126A

Code

English

1H-INDOLE-4-CARBOXAMIDE, N-((1,2-DIHYDRO-4,6-DIMETHYL-2-OXO-3-PYRIDINYL)METHYL)-3-METHYL-1-((1S)-1-METHYLPROPYL)-6-(6-(1-PIPERAZINYL)-3-PYRIDINYL)-

Systematic Name

English

GSK 2816126 [WHO-DD]

Common Name

English

(S)-1-(SEC-BUTYL)-N-((4,6-DIMETHYL-2-OXO-1,2-DIHYDROPYRIDIN-3-YL)METHYL)-3-METHYL-6-(6-(PIPERAZIN-1-YL)PYRIDIN-3-YL)-1H-INDOLE-4-CARBOXAMIDE

Systematic Name

English

N-((1,2-DIHYDRO-4,6-DIMETHYL-2-OXO-3-PYRIDINYL)METHYL)-3-METHYL-1-((1S)-1-METHYLPROPYL)-6-(6-(1-PIPERAZINYL)-3-PYRIDINYL)-1H-INDOLE-4-CARBOXAMIDE

Systematic Name

English

Code System Code Type Description

FDA UNII

W4OGW9QZ97